Features and properties of finafloxacin Alternative names BY 377; BY-377; finafloxacin

hydrochloride; gastrochinolon; gastroquinolone; XtoroTM Class Fluoroquinolone, small-

molecule Mechanism of action DNA gyrase inhibitor; DNA topoisomerase IV inhibitor
Route of administration Topical, oral, intravenous Antimicrobial activity Antimicrobial
activity enhanced in acidic versus neutral conditions against multiple species, including skin
and urinary pathogens. Superior antibacterial activity to that of other fluoroquinolones in
acidic conditions (pH 5.8) against multiple species. Longer post-antibacterial effect than
other fluoroquinolones under acidic conditions against multiple species. Resistance is less
likely in acidic than neutral conditions Pharmacodynamics Highly selective for bacterial type
II topoisomerases (i.e. DNA gyrase and topoisomerase IV); broad spectrum of antibacterial
activity Pharmacokinetics After repeated topical administration (finafloxacin otic suspension
0.3 %, 4 drops each ear for 7 days), quantifiable plasma concentrations were observed in 2 of
36 healthy subjects. After oral administration, the drug is well absorbed, reaching peak
plasma levels in just under 1 h Adverse events Occasional (topical) Ear pruritus, nausea
Occasional (oral and intravenous) Diarrhoea, nausea, fatigue, headache, injection site
reactions, musculoskeletal disorders ATC codes WHO ATC code A02B-X (Other drugs for
peptic ulcer and gastro-oesophageal reflux disease), J01 M-A (Fluoroquinolones), S02A
(Anti-infectives) EphMRA ATC code A2B9 (all other anti-ulcerants), J1G1 (oral
fluoroquinolones), J1G2 (injectable fluoroquinolones), S2A (otic anti-infectives) Chemical
name (-)-8-Cyano-1-cyclopropyl-6-fluoro-7-((4aS,7aS)-hexahydropyrrolo(3,4-b)-1,4-oxazin-
6(2H)-yl)- 4-oxo-1,4-dihydroquinoline-3-carboxylic acid

https://sci-hub.se/10.1007/s40265-015-0384-z

Pharmacokinetics Plasma pharmacokinetics of finafloxacin was analyzed after orally

administered single doses of 25, 50, 100, 200, 400 and 800 mg. The Cmax values were: 0.24,
0.44 ± 0.16, 1.32 ± 0.62, 1.90 ± 0.73, 5.06 ± 2.09 and 11.1 ± 2.96 mg/L, respectively.
The half life-time of finafloxacin in single dose administration were as follows: 1.28,
3.8 ± 2.7, 7.2 ± 3.2, 4.6 ± 1.9, 10.0 ± 4.4 and 10.5 ± 2.2 h, respectively. The time to reach the
Cmax varied between 0.5 and 1 h. In the case of multiple doses of 150, 300, 600 and 800 mg
were administered orally once daily for seven consecutive days. The Cmax after the seventh
day showed the following concentrations: 1.50 ± 0.52, 4.15 ± 2.11, 6.76 ± 2.2 and
8.95 ± 3.11 mg/L. The corresponding halflife time was 5.3 ± 0.6, 6.5 ± 2.5, 8.8 ± 3.1 and
14 ± 5.5 h, respectively. While time to reach Cmax was between 0.5 and 1.5 h [19].
Accumulation of finafloxacin was not relevant following daily once application of doses up
to 800 mg over 7 days. Peak serum concentrations may slightly increase proportionally
compared to dose [19]. The urine recovery data show that around 30 % of oral dose can be
detected. Moreover, the urine finafloxacin concentration exceeds MIC values determined in
Mueller–Hinton broth for many pathogens of urinary tract infections e.g.,: E. coli and P.
aeruginosa. This feature makes it advantageous in treatment of several urinary tract infections
[21, 22]. The mean concentration of finafloxacin in urine was 68 mg/L in the first 4 h and
4 mg/L at the time of 12–24 h sampling following 200 mg dose. In the case of the 800 mg
dose the mean finafloxacin concentration was 112 mg/L in the first 4 h (peak of 150 mg/L
was reached in the 4–8 h interval) and 18 mg/L in the 12–24 h sampling period [23].

Bismillah hayuukk

https://www.merlionpharma.com/wp-content/uploads/2014/03/F1-2036_Wohlert.pdf

https://www.merlionpharma.com/news-publications/presentations-and-posters/

10.1128/AAC.00082-17

formula :
https://patents.google.com/patent/US8536167B2/en

sintetis
https://sci-hub.tw/10.1021/op100229b